Zotarolimus is an analog made by substituting a tetrazole ring in abode of the built-in hydroxyl accumulation at position 42 in rapamycin that is abandoned and antiseptic as a accustomed artefact from fermentation. This website of modification was begin to be the a lot of advanced position to acquaint atypical structural changes after impairing drug activity.
The admixture is acutely lipophilic, with a actual top octanol:water allotment coefficient, and accordingly has bound baptize solubility. These backdrop are awful advantageous for designing a drug-loaded stent absolute zotarolimus in adjustment to access a apathetic abiding absolution of drug from the stent anon into the bank of coronary vessels. The poor baptize solubility prevents accelerated absolution into the circulation, back elution of drug from the stent will be partly dissolution rate-limited. The apathetic amount of absolution and consecutive circulation of the atom facilitates the aliment of ameliorative drug levels eluting from the stent.
In addition, its lipophilic appearance favors bridge corpuscle membranes to arrest neointimal admeasurement of ambition tissue. The octanol:water allotment coefficients of a amount of compounds, afresh acquired in a allusive study, announce that zotarolimus is the a lot of lipophilic of all DES drugs.